A novel route for the synthesis of thiazolo[3,2-a]pyrimidin-7-ones and pyrido[1,2-a]pyrimidin-2,ones from acetylated 2- aminothiazoles and 2-aminopyridines under Vilsmeier conditions has been developed. The plausible ...A novel route for the synthesis of thiazolo[3,2-a]pyrimidin-7-ones and pyrido[1,2-a]pyrimidin-2,ones from acetylated 2- aminothiazoles and 2-aminopyridines under Vilsmeier conditions has been developed. The plausible mechanism has also been proposed.展开更多
A series of（Z）-2-chloro-1,3-diarylpropen-1-ones were unexpectedly synthesized in moderate yields by treatment of easily available 2,3-epoxy-1,3-diarylpropan-1-ones with Vilsmeier reagent,which was derived from bis（...A series of（Z）-2-chloro-1,3-diarylpropen-1-ones were unexpectedly synthesized in moderate yields by treatment of easily available 2,3-epoxy-1,3-diarylpropan-1-ones with Vilsmeier reagent,which was derived from bis（trichloromethyl） carbonate（BTC, triphosgene） and DMF.A possible mechanism was also proposed,where sequential ring-opening,halogenation and elimination reactions were involved.展开更多
Thifensulfuron was synthesized in two steps by reacting bis(trichloromethyl)carbonate(BTC) as a phosgene substitute with 2 methoxycarbonyl 3 aminosulfonylthiophene(AST) to give an intermediate sulfonylisocynate, which...Thifensulfuron was synthesized in two steps by reacting bis(trichloromethyl)carbonate(BTC) as a phosgene substitute with 2 methoxycarbonyl 3 aminosulfonylthiophene(AST) to give an intermediate sulfonylisocynate, which reacted with 2 amino 4 methoxy 6 methyl 1,3,5 triazine to give thifensulfuron. The optimum reaction conditions were n (AST)∶ n (BTC)=1∶0 56, reaction temperature 120～130 ℃ and reaction time (11±0 5) h. The purity of thifensulfuron obtained was 96 5%(HPLC) in overall yield 93%.展开更多
基金Zhejiang Key Innovation Team of Green Pharmaceutical Technology (Project No.:2012R20043-12)
文摘A novel route for the synthesis of thiazolo[3,2-a]pyrimidin-7-ones and pyrido[1,2-a]pyrimidin-2,ones from acetylated 2- aminothiazoles and 2-aminopyridines under Vilsmeier conditions has been developed. The plausible mechanism has also been proposed.
基金the National Natural Science Foundation of China(Nos.20806073 and 20876147)the National Key Technology Research and Development Program(No.2007BAI34B06) for financial support
文摘A series of（Z）-2-chloro-1,3-diarylpropen-1-ones were unexpectedly synthesized in moderate yields by treatment of easily available 2,3-epoxy-1,3-diarylpropan-1-ones with Vilsmeier reagent,which was derived from bis（trichloromethyl） carbonate（BTC, triphosgene） and DMF.A possible mechanism was also proposed,where sequential ring-opening,halogenation and elimination reactions were involved.
文摘Thifensulfuron was synthesized in two steps by reacting bis(trichloromethyl)carbonate(BTC) as a phosgene substitute with 2 methoxycarbonyl 3 aminosulfonylthiophene(AST) to give an intermediate sulfonylisocynate, which reacted with 2 amino 4 methoxy 6 methyl 1,3,5 triazine to give thifensulfuron. The optimum reaction conditions were n (AST)∶ n (BTC)=1∶0 56, reaction temperature 120～130 ℃ and reaction time (11±0 5) h. The purity of thifensulfuron obtained was 96 5%(HPLC) in overall yield 93%.
